EP3646873A1 - Folatsalze - Google Patents

Folatsalze Download PDF

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Publication number
EP3646873A1
EP3646873A1 EP18203849.7A EP18203849A EP3646873A1 EP 3646873 A1 EP3646873 A1 EP 3646873A1 EP 18203849 A EP18203849 A EP 18203849A EP 3646873 A1 EP3646873 A1 EP 3646873A1
Authority
EP
European Patent Office
Prior art keywords
folate
tetrahydrofolic acid
crystalline
salt according
anion
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP18203849.7A
Other languages
English (en)
French (fr)
Inventor
Martin Ulmann
Gerd WIESLER
Arthur BODENMÜLLER
Markus Müller
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aprofol AG
Original Assignee
Aprofol AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Aprofol AG filed Critical Aprofol AG
Priority to EP18203849.7A priority Critical patent/EP3646873A1/de
Priority to BR112021008325-1A priority patent/BR112021008325A2/pt
Priority to CN201980072059.2A priority patent/CN113056273A/zh
Priority to EP19801774.1A priority patent/EP3873475A1/de
Priority to CA3117575A priority patent/CA3117575A1/en
Priority to US17/289,609 priority patent/US11787808B2/en
Priority to JP2021523460A priority patent/JP2022506246A/ja
Priority to PCT/EP2019/079941 priority patent/WO2020089443A1/en
Priority to AU2019370731A priority patent/AU2019370731A1/en
Publication of EP3646873A1 publication Critical patent/EP3646873A1/de
Priority to US18/243,991 priority patent/US20230416253A1/en
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Nutrition Science (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EP18203849.7A 2018-10-31 2018-10-31 Folatsalze Withdrawn EP3646873A1 (de)

Priority Applications (10)

Application Number Priority Date Filing Date Title
EP18203849.7A EP3646873A1 (de) 2018-10-31 2018-10-31 Folatsalze
US17/289,609 US11787808B2 (en) 2018-10-31 2019-10-31 Folate salts
CN201980072059.2A CN113056273A (zh) 2018-10-31 2019-10-31 叶酸盐
EP19801774.1A EP3873475A1 (de) 2018-10-31 2019-10-31 Folatsalze
CA3117575A CA3117575A1 (en) 2018-10-31 2019-10-31 Folate salts
BR112021008325-1A BR112021008325A2 (pt) 2018-10-31 2019-10-31 sais de folato
JP2021523460A JP2022506246A (ja) 2018-10-31 2019-10-31 葉酸塩
PCT/EP2019/079941 WO2020089443A1 (en) 2018-10-31 2019-10-31 Folate salts
AU2019370731A AU2019370731A1 (en) 2018-10-31 2019-10-31 Folate salts
US18/243,991 US20230416253A1 (en) 2018-10-31 2023-09-08 Folate salts

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP18203849.7A EP3646873A1 (de) 2018-10-31 2018-10-31 Folatsalze

Publications (1)

Publication Number Publication Date
EP3646873A1 true EP3646873A1 (de) 2020-05-06

Family

ID=64048998

Family Applications (2)

Application Number Title Priority Date Filing Date
EP18203849.7A Withdrawn EP3646873A1 (de) 2018-10-31 2018-10-31 Folatsalze
EP19801774.1A Pending EP3873475A1 (de) 2018-10-31 2019-10-31 Folatsalze

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP19801774.1A Pending EP3873475A1 (de) 2018-10-31 2019-10-31 Folatsalze

Country Status (8)

Country Link
US (2) US11787808B2 (de)
EP (2) EP3646873A1 (de)
JP (1) JP2022506246A (de)
CN (1) CN113056273A (de)
AU (1) AU2019370731A1 (de)
BR (1) BR112021008325A2 (de)
CA (1) CA3117575A1 (de)
WO (1) WO2020089443A1 (de)

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0626965A1 (de) * 1992-02-20 1994-12-07 BRACCO S.p.A. Verfahren zur trennung von stereoisomere von folinsäure
US5382581A (en) * 1990-04-12 1995-01-17 Sapec S.A. Fine Chemicals (6R)- and (6S)-diastereoisomers of an ammonium salts of N5 -methyl-5,6,7,8-tetrahydrofolic acid
US5710271A (en) * 1994-06-08 1998-01-20 Dibra S.P.A. Process for the preparation and separation of diastereomeric salts of folinic acid
US5817659A (en) 1995-11-07 1998-10-06 Eprova Ag Stable crystalline tetrahydrofolic acid salts
US6441168B1 (en) 1999-04-15 2002-08-27 Eprova Ag Stable crystalline salts of 5-methyltetrahydrofolic acid
WO2009103333A1 (en) * 2008-02-20 2009-08-27 Gnosis S.P.A. Process for the diastereoisomeric resolution of 5-methyltetrahydrofolic acid
WO2009103334A1 (en) * 2008-02-20 2009-08-27 Gnosis S.P.A. Folates, compositions and uses thereof
US9301922B1 (en) 2013-04-30 2016-04-05 Aprofol Ag Stable high strength pharmaceutical composition of levoleucovorin
US20160207925A1 (en) * 2013-12-31 2016-07-21 Gianni Fracchia L-methylfolate salt preparations, medicaments, and nutritional supplements comprising such salts thereof
US9642853B2 (en) 2013-04-30 2017-05-09 Aprofol Ag Stable pharmaceutical composition containing folates
CN107304212A (zh) * 2016-04-21 2017-10-31 常州爱诺新睿医药技术有限公司 一种无定型l-5-甲基四氢叶酸氨基酸盐及其制备方法
WO2018178142A1 (en) * 2017-03-31 2018-10-04 Merck Patent Gmbh Crystalline binary sodium salts of 5-methyl-(6s)-tetrahydrofolic acid with organic bases

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2766324T3 (es) * 2013-09-06 2020-06-12 Res Found Dev Formas salinas de Alfa-TEA: composiciones y usos para tratar enfermedades
EP3461826A1 (de) * 2017-09-29 2019-04-03 Aprofol AG Multifunktionelle folatsalze
EP3616700A1 (de) * 2018-08-29 2020-03-04 Aprofol AG Folatpräparate zur behandlung von augenerkrankungen

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5382581A (en) * 1990-04-12 1995-01-17 Sapec S.A. Fine Chemicals (6R)- and (6S)-diastereoisomers of an ammonium salts of N5 -methyl-5,6,7,8-tetrahydrofolic acid
EP0626965A1 (de) * 1992-02-20 1994-12-07 BRACCO S.p.A. Verfahren zur trennung von stereoisomere von folinsäure
US5710271A (en) * 1994-06-08 1998-01-20 Dibra S.P.A. Process for the preparation and separation of diastereomeric salts of folinic acid
US5817659A (en) 1995-11-07 1998-10-06 Eprova Ag Stable crystalline tetrahydrofolic acid salts
US6441168B1 (en) 1999-04-15 2002-08-27 Eprova Ag Stable crystalline salts of 5-methyltetrahydrofolic acid
WO2009103333A1 (en) * 2008-02-20 2009-08-27 Gnosis S.P.A. Process for the diastereoisomeric resolution of 5-methyltetrahydrofolic acid
WO2009103334A1 (en) * 2008-02-20 2009-08-27 Gnosis S.P.A. Folates, compositions and uses thereof
US9301922B1 (en) 2013-04-30 2016-04-05 Aprofol Ag Stable high strength pharmaceutical composition of levoleucovorin
US9642853B2 (en) 2013-04-30 2017-05-09 Aprofol Ag Stable pharmaceutical composition containing folates
US20160207925A1 (en) * 2013-12-31 2016-07-21 Gianni Fracchia L-methylfolate salt preparations, medicaments, and nutritional supplements comprising such salts thereof
CN107304212A (zh) * 2016-04-21 2017-10-31 常州爱诺新睿医药技术有限公司 一种无定型l-5-甲基四氢叶酸氨基酸盐及其制备方法
WO2018178142A1 (en) * 2017-03-31 2018-10-04 Merck Patent Gmbh Crystalline binary sodium salts of 5-methyl-(6s)-tetrahydrofolic acid with organic bases

Also Published As

Publication number Publication date
BR112021008325A2 (pt) 2021-08-03
CA3117575A1 (en) 2020-05-07
US20230416253A1 (en) 2023-12-28
EP3873475A1 (de) 2021-09-08
AU2019370731A1 (en) 2021-05-27
US20210403471A1 (en) 2021-12-30
US11787808B2 (en) 2023-10-17
CN113056273A (zh) 2021-06-29
JP2022506246A (ja) 2022-01-17
WO2020089443A1 (en) 2020-05-07

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